Computer Aided Formulation and Characterization of Propranolol Hcl Buccal Tablet Using Polymeric Blend

Abstract

Abstract:The current study was aimed to formulate a continuous release mucoadhesive buccal tablet containing propranolol HCl. The type and quantities of polymers as well as method of compression were set in a preliminary study (F1-F13). Direct compression method was employed in the main study (F14-F24) using Carbopol ® 934P (CP), ethylcellulose (EC), sodium alginate (SA), hydroxypropyl methylcellulose (HPMC k4M) and carboxymethylcellulose (CMC) as mucoadhesive polymers and were tested for physicochemical tests i.e. swellability, surface pH, mucoadhesive time, mucoadhesive strength, in vitro release etc. Results obtained from the study were optimized using NeuralPower ® 3.1, an artificial intelligence approach. Against the desirability of physicochemical parameters, the software optimized the ingredients as HPMC (150mg), CMC (25mg), CP (20mg) and EC (20mg). Outcome revealed that HPMC primarily contributed to the physicochemical properties of mucoadhesive formulation. To compare prediction, optimized ingredients were formulated (F25) and tested. The swellability index of confirmation formulation (F25) was 102% at 6 h. As predicted, similar release pattern was of F25 was obtained as 26% (0.5h), 34% (1h), 40% (2h), 45% (3h), 50% (4h), 62% (5h), 76% (6h), 85% (7h) and 97% (8h) respectively. For release kinetics, DD solver ® suggested the release of the drug to be non-Fickian.

Exorbitant Drug Loading of Metformin and Sitagliptin in Mucoadhesive Buccal Tablet: In Vitro and In Vivo Characterization in Healthy Volunteers

“…These were subjected to be weighed individually and the average weight for each formulation was calculated to estimate the standard deviation. Thickness and diameter were calculated using digital Vernier caliper on the formulated tablets and the results were expressed in terms of standard deviation [12], while hardness was determined by using automated hardness tester Curio HT-901 on ten tablets. The friability was estimated by Roche friabilator ® (Scientific Supplies, Karachi, Pakistan) wherein approximately 6.6 g of sample was placed in a friabilator at 25 rpm for 4 min.…”

“…Afterwards, one face of the tablet was wetted with approximately 500 µL of PBS and was then pressed gently for few seconds on the excised tissue to fix mucoadhesive tablet for ET evaluation [11]. Thereafter, glass slide containing attached tablet was immersed in the beaker at an angle of 45 • containing 900 mL of phosphatebuffered solution (PBS), adjusted to pH 6.8 with phosphoric acid [12]. The temperature of the apparatus was maintained at 37 • C during the experiment with a stirring speed of 100 rpm.…”

“…When the system was stable, weight was added in the other pan. The mass (g) at which the tablets detached from the mucosa was considered as a mucoadhesive strength [12]. [31], where 1 = moveable glass slide with attached mucosa, 2 = attached mucosa to fixed glass slide to 3 = base, 4 = modified arm and 5 = weight added to the other arm.…”

“…Therefore, we addressed these concerns in our research via the formulation of buccal mucoadhesive tablets to ensure sustained systemic drug release with a low frequency of dosing [10]. Buccal mucoadhesive drug delivery has attained considerable interest in delivering local as well as systemic drug release [11,12] via the localization of the dosage form to the buccal cavity for drug absorption [11,13]. Moreover, localized intra-pocket, retentive, biodegradable, prolonged release buccal mucoadhesive tablets can provide an improved therapeutic efficacy of doxycycline at the site of action while evading off target side effects [10].…”

Assessment of Binary Agarose–Carbopol Buccal Gels for Mucoadhesive Drug Delivery: Ex Vivo and In Vivo Characterization

“…When the whole system was static and stable, weight on the left pan was added as drops of water to generate tension on the thread. As the tension increased, the force at which the gel was detached from either surface of the buccal mucosa was considered the MS value [ 64 , 65 ].…”